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Advancing Aptamer Applications™

Aptamers"synthetic" antibodies

Apta-beacons &Apta-sensors

Peptimers™(Apta-peptides)

Aptabodies™(NextGEN Aptamers)

WHAT ARE APTAMERS?

Aptamers (synthetic antibodies) are stable ssDNA or RNA ligands that bind with high affinity and specificity to target antigens such as small molecules, peptides, proteins, cells, and tissues. For example, aptamers have been generated that exhibit greater than 10,000-fold binding affinity for theophylline over caffeine, which differ only by a few atoms. Aptamer products can be used as research reagents, diagnostics, biosensors, and tools for biomarker or drug discovery. Aptamers can also be used for bioindustrial applications and targeted therapeutics.

What are Aptamers?

What is an aptamer? A stable DNA, RNA, or peptide that binds with high affinity and specificity to targets such as small organics, peptides, proteins, cells, and tissues. For example, search our Apta-Index™ (Aptamer Database).

Unlike antibodies, some aptamers exhibit stereoselectivity. In addition, aptamers (synthetic antibodies) have been generated that exhibit greater than 10,000-fold binding affinity for theophylline over caffeine, which differ from one another in structure by only a single methyl group.

Diagnostics

Aptamers (synthetic antibodies) are (stable) single-stranded DNA, RNA, or peptide molecules capable of binding to its target antigen with high affinity and specificity. Aptamers (synthetic antibodies) have been developed against a wide variety of targets ranging from small organics to large proteins.

Benefits

Manufacturing costs and time are all lower compared to that of monoclonal antibody production.

Once the aptamer (nucleic acid) sequence is known, the aptamer (synthetic antibody) can be produced on the fly using an oligo synthesizer to meet ones immediate needs.

Targeting

Using the current antibody method; for every drug that makes it to market, hundreds of promising candidates that worked in-vitro (on the lab bench) fail during animal ADMET studies (absorption, distribution, metabolism, excretion, and toxicity). From lab bench to pharmacy shelves it takes from seven to fifteen years and costs $4B with an average failure rate of 80%. Half of this time and approximately 70% of all associated biopharmaceutical R&D costs are spent on in-vitro development.

Because aptamers (synthetic antibodies) are an in-vivo (directly tested in the animal model) approach, they avoid the majority of the bench testing, saving several years and approximately 35% of the R&D cost. The unique chemistry of aptamers, unlike other forms of drugs currently used, permits the natural selection of drug candidates in whole animal models, bypassing the test tube entirely. By using an animal model with the disease state of interest, Aptagen need not possess specific knowledge of the pathology or disease condition in question. As an added benefit, because this approach reduces the false starts, there are actually fewer animals needed for drug evaluation.

The Problem: Drug candidates that prove positive in "test tube" (or in vitro) assays may face substantial problems when tested in animals, a necessary prerequisite before human clinical trials. These problems include absorption, distribution, metabolism, excretion, and toxicity.

The Solution: Aptagen's technique, involving molecules called aptabodies™ (patent pending), overcomes the limitation of the traditional pharmaceutical drug discovery process. The unique chemistry of aptabodies™, unlike other forms of drugs currently used, permits the selection of drug candidates in whole animal models, bypassing the "test tubes" entirely, and taking drug development one step closer to human clinical trials. By using an animal model with the disease state of interest, specific knowledge of the pathology or disease condition is not needed. An added benefit is the significant reduction in the number of animals needed for drug evaluation before entering into human clinical trials.

Spending too much time and capital on the trial-and-error approach to Drug Discovery? On average, only one in a thousand drug candidates make it to human clinical trials. The cost and time associated with the traditional method of drug development is expensive and quite slow (7 to 15 years and almost $1 Billion). However, Aptagen's technology significantly reduces the unpredictability, cost, and time for drug discovery and development.

Over a century ago, Paul Ehrlich described the ideal drug, famously known as a 'magic bullet,' in which it specifically targets the disease site and would not harm healthy tissue. However, finding these magic bullets with drug-like properties involves a trial and error approach and is extremely slow. Aptagen has developed the concept of a ‘replicating magic bullet’ called an aptabody™. The aptabody™ technology has a shorter development time compared to traditional methods of drug development, and can be used to increase the specificity and improve delivery of existing drug compounds resulting in the next generation of pharmaceuticals with improved pharmacodynamics and pharmacokinetics.

Contact us for more information on how we can solve your drug pipeline needs.

No Capturing. No Washing. Just READ....In Minutes!

Aptagen’s "No Capturing. No Washing. Just READ" assay is a radical advancement in diagnostic technology. Aptagen, LLC has developed a sensitive diagnostic platform that can detect virtually any target or antigen (from small molecules to protein biomarkers and cells) in a variety of sample matrices. Unlike current diagnostic formats, such as the traditional ELISA method and the more recently popular Luminex® approach, Aptagen’s Apta-Beacon™ assay eliminates the need for multiple target manipulation steps. The Apta-Beacon™ platform requires neither capturing nor washing of sample(s), streamlining the analysis to quickly provide results with higher sensitivity.

The demo kit showcases the specificity of the colorimetric assay by detecting difficult small molecule targets, theophylline versus caffeine, which only differ by a single methyl group. The assay is also available in a fluorescent format for greater sensitivity.

What are Peptimers™?

Peptimers™ are
peptide-based aptamers: high affinity ligands composed of amino acid building
blocks instead of the nucleic acid bases that make up RNA or DNA
aptamers. Peptimers™ are another option offered by Aptagen to continually
‘Advance Aptamer Applications’. Unlike peptides or single-chain
antibodies generated by the phage display or biopanning process, peptimers™ are
discovered through a process similar to aptamer SELEX, called mRNA
display.

Contact Us for more information on how peptimers™ may meet your
application needs.

WHAT IS AN APTABODY™?

An aptabody™ is a supramolecular form of an aptamer ligand containing a wide variety of functional groups. The aptamer component acts as a scaffold to hold into place one or more functional groups such as amino acids, fatty acids, carbohydrates, small molecules and/or metals in a unique orientation in 3-D space. The order and proximity of these functional groups play a role in enhanced functionalities ranging from higher affinity and specificity over “naked” aptamers, to enzyme biomimetics, improved molecular targeting in vivo, cellular trafficking, pharmacokinetics/dynamics, and drug-like properties.

What are Aptabodies™?

Aptamers are best leveraged as research reagents or as diagnostic elements in biosensor platforms. Aptamers are not mature enough for therapeutics; however, they can be used for targeting, as the vehicle to deliver a drug payload. To overcome the limitations of aptamers as drug candidates, Aptagen has conceptualized the Aptabody™ for the therapeutic area.

What is an aptabody™? An aptabody™ is a supramolecular form of an aptamer ligand containing a wide variety of functional groups. The aptamer component acts as a scaffold to hold into place one or more functional groups such as amino acids, fatty acids, carbohydrates, small molecules and/or metals into a unique orientation in 3-D space. The order and proximity of these functional groups play a role in enhanced functionalities ranging from higher affinity and specificity over “naked” aptamers, to enzyme biomimetics, improved molecular targeting in vivo, cellular trafficking, pharmacokinetics/dynamics, and drug-like properties.

NOTE: Conventional antibodies have a chemical alphabet of the naturally occurring amino acids. Aptabodies™, by definition, have a chemical alphabet of all amino acids, fatty acids, sugars, as well as synthetic compounds, co-factors, metal ions, etc...

Can aptabodies represent a class of artificial enzymes, biomaterials, and nanomaterials? Contact Us.

Aptagen develops and manufactures aptamers (synthetic antibodies) which are ligands of RNA, DNA, and peptide oligos that bind to a variety of target antigens. Aptamers (synthetic antibodies) are sometimes referred to as "chemical antibodies or DNA antibodies." Aptazymes are aptamers (synthetic antibodies) with enzymatic activity. A subclass of aptazymes called molecular switches is analogous to molecular beacons for fluorescent detection of analytes in test samples. Examples include allosteric ribozymes, also known as riboswitches.

Allosteric ribozymes (or riboswitches) have been engineered to act like molecular switches turning "on" or "off" in the presence or absence of effectors. Ribozyme catalysis is modulated by rapid conformational changes imparted by an effector molecule binding to an aptamer domain apart from the catalytic site. The aptamer domain is a structural region of several nucleotides that binds specifically to its cognate effector molecule. With the advent of allosteric RNA switches and aptazymes, it was soon recognized that the precise molecular recognition and high degree of selectively exhibited by these molecules make them ideal biosensor elements which can be immobilized on a solid support for microarray analysis and biosensor applications. Compared to other types of biosensor recognition elements such as proteins, antibodies, and oligonucleotides, which are commonly used in microarrays to detect a narrow assortment of targets, RNA allosteric elements are better suited for the detection of a wide variety of analytes in a complex mixture, since unlike proteins, antibodies, and oligonucleotides, they are not limited by the types of targets they can bind. As described before, the ability to rapidly develop RNA molecular switches using one pot selection techniques against a vast array of targets permits the rapid development of biochips capable of analyzing and fingerprinting a complex mixture of chemical and biological targets. The versatility and utility of these molecular switches have been employed in biochips which are able to detect specific targets from a complex mixture containing metal ions, enzyme cofactors, metabolites, serum biomarkers, drug analytes, and strains of E coli strain from culture media.

Aptagen, LLC is a biotechnology company offering aptamer (synthetic antibody) products and services as research reagents, diagnostic and biomarker discovery tools, as well as for use in drug discovery and targeted delivery for therapeutics, and bioindustrial applications. We have 20 years of experience in developing aptamers (synthetic antibodies) for all types of downstream applications.